Copper-Catalyzed Oxidative Cascade Inter-Molecular Double Cyclization of 2-Iodobenzamide Derivatives and Propargyl Dicarbonyl Compounds for Accessing 3-Hydroxy-3-Furylisoindolinone Derivatives

A one-pot strategy for the synthesis of 3-hydroxy-3-furylisoindolinone derivatives is reported. The reaction proceeds via a copper-catalyzed oxidative cascade inter-molecular double cyclization of 2-iodobenzamide derivatives and propargyl dicarbonyl compounds in the presence of oxygen. The strategy involves several reactions including cyclization/coupling/double C(sp3)−H functionalization in a cascade manner. A wide range of 2-iodobenzamide substrates containing different substituents as well as various propargyldicarbonyl compounds and propargylsulfonyl aryl ketones can be used to access a variety of 3-hydroxy-3-furylisoindolinone derivatives. (Figure presented.).